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TL02-59 dihydrochloride is an orally active inhibitor of the Src-family kinase Fgr, with an IC50 of 0.03 nM.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | $1,120 | 35 days | 35 days | |
| 50 mg | $4,690 | 35 days | 35 days |
| Description | TL02-59 dihydrochloride is an orally active inhibitor of the Src-family kinase Fgr, with an IC50 of 0.03 nM. |
| Targets&IC50 | Hck:160 nM , FGR:0.03 nM , Lyn:0.1 nM |
| In vitro | in TF-1 cells, TL02-59 dihydrochloride (0.1-1000 nM; 6 hours) potently inhibits Fgr autophosphorylation , with paritial inhibition at 0.1-1 nM and complete inhibition above 10 nM. Hck, Lyn and Flt3 are inhibited in the 100 to 1000 nM range. TL02-59 dihydrochloride induces growth arrest in primary AML bone marrow samples. TL02-59 dihydrochloride inhibits the growth and induced apoptosis of AML cell lines expressing this kinase with single-digit nM potency. |
| In vivo | TL02-59 (oral; 1 and 10 mg/kg; for three weeks) entirely eliminates AML cells from the spleen and peripheral blood in a mouse model of AML, while significantly suppressing bone marrow involvement. |
| Molecular Weight | 682.56 |
| Formula | C32H36Cl2F3N5O4 |
| Cas No. | 2415263-06-6 |
| Smiles | O=C(C1=CC=C(C)C(OC2=NC=NC3=C2C=C(OC)C(OC)=C3)=C1)NC4=CC=C(CN5CCN(CC5)CC)C(C(F)(F)F)=C4.Cl.Cl |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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